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Assay Detail

CHEMBL1820399

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of HDAC1
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Histone deacetylase 1 (CHEMBL325)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors.
Shultz MD, Cao X, Chen CH, Cho YS, Davis NR, Eckman J, Fan J, Fekete A, Firestone B, Flynn J, Green J, Growney JD, Holmqvist M, Hsu M, Jansson D, Jiang L, Kwon P, Liu G, Lombardo F, Lu Q, Majumdar D, Meta C, Perez L, Pu M, Ramsey T, Remiszewski S, Skolnik S, Traebert M, Urban L, Uttamsingh V, Wang P, Whitebread S, Whitehead L, Yan-Neale Y, Yao YM, Zhou L, Atadja P.
J Med Chem (2011) 54 : 4752 -4772
PubMed 21650221 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 7.99 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1819273 1 9.00
CHEMBL1819274 1 9.00
CHEMBL1819257 1 8.89
CHEMBL1819267 1 8.82
CHEMBL1819272 1 8.70
CHEMBL1819260 1 8.70
CHEMBL1819275 1 8.52
CHEMBL1819270 1 8.52
CHEMBL1819261 1 8.40
CHEMBL1819266 1 8.30
CHEMBL1819271 1 8.22
CHEMBL1819269 1 8.22
CHEMBL1819264 1 8.10
CHEMBL1819268 1 8.00
CHEMBL1819262 1 7.96
CHEMBL1819256 1 7.92
CHEMBL1819141 1 7.92
CHEMBL1819255 1 7.92
CHEMBL1819138 1 7.89
CHEMBL356066 DACINOSTAT 2.0 1 7.82
CHEMBL344227 1 7.82
CHEMBL1819259 1 7.77
CHEMBL1819265 1 7.68
CHEMBL1819137 1 7.66
CHEMBL142992 1 7.64
CHEMBL1819254 1 7.64
CHEMBL1819263 1 7.51
CHEMBL1819143 1 7.33
CHEMBL1819258 1 7.31
CHEMBL1819139 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1819273 IC50 = 1.0 nM 9.00
CHEMBL1819274 IC50 = 1.0 nM 9.00
CHEMBL1819257 IC50 = 1.3 nM 8.89
CHEMBL1819267 IC50 = 1.5 nM 8.82
CHEMBL1819272 IC50 = 2.0 nM 8.70
CHEMBL1819260 IC50 = 2.0 nM 8.70
CHEMBL1819275 IC50 = 3.0 nM 8.52
CHEMBL1819270 IC50 = 3.0 nM 8.52
CHEMBL1819261 IC50 = 4.0 nM 8.40
CHEMBL1819266 IC50 = 5.0 nM 8.30
CHEMBL1819271 IC50 = 6.0 nM 8.22
CHEMBL1819269 IC50 = 6.0 nM 8.22
CHEMBL1819264 IC50 = 8.0 nM 8.10
CHEMBL1819268 IC50 = 10.0 nM 8.00
CHEMBL1819262 IC50 = 11.0 nM 7.96
CHEMBL1819141 IC50 = 12.0 nM 7.92
CHEMBL1819255 IC50 = 12.0 nM 7.92
CHEMBL1819256 IC50 = 12.0 nM 7.92
CHEMBL1819138 IC50 = 13.0 nM 7.89
CHEMBL356066 DACINOSTAT IC50 = 15.0 nM 7.82
CHEMBL344227 IC50 = 15.0 nM 7.82
CHEMBL1819259 IC50 = 17.0 nM 7.77
CHEMBL1819265 IC50 = 21.0 nM 7.68
CHEMBL1819137 IC50 = 22.0 nM 7.66
CHEMBL142992 IC50 = 23.0 nM 7.64
CHEMBL1819254 IC50 = 23.0 nM 7.64
CHEMBL1819263 IC50 = 31.0 nM 7.51
CHEMBL1819143 IC50 = 47.0 nM 7.33
CHEMBL1819258 IC50 = 49.0 nM 7.31
CHEMBL1819139 IC50 = 120.0 nM 6.92
CHEMBL1819142 IC50 = 130.0 nM 6.89
CHEMBL1819140 IC50 = 210.0 nM 6.68